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Advance in Antitumor Agents Targeting Glutathione-S-Transferase

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Glutathione-S-transferases (GSTs; EC 2.5.1.18), a family of phase II detoxification enzymes, catalyze the conjugation of glutathione with broad substrates including chemotherapeutic agents, and are involved in cell protection against apoptotic signals by inhibiting the stress-signaling cascade mediated by ASK1 (Apoptosis signal-regulating kinase)-JNK (c-Jun N-terminal kinase). As GSTs are overexpressed in some malignant tumors, GSTs is a promising therapeutic target. This article reviews the progress in the development of GSTs inhibitors and GSTs activated prodrugs.
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Keywords: Antitumor agents; Apoptosis; Drug-resistance; GST inhibitors; Glutathione-S-transferases; Prodrugs

Document Type: Research Article

Affiliations: Department of Medicinal Chemistry, College of Pharmacy, Shandong University, Jinan, Shandong 250012, PR China.

Publication date: 2006-05-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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